This invention relates to N-[2-dimethylamino)ethyl]-N'-[3- [3-[(1- piperidinyl)methyl]phenoxyl]propyl]-1,2,5-thiadiazole-3,4-diamine, 1-oxide, the object compound of this invention. The object compound has the following formula: ##STR1## The invention also relates to a process for preparing the compound, to a pharmaceutical formulation thereof, and to methods of using the compound.
R. R. Crenshaw and A. A. Algieri, U.K. Patent Application No. 2,067,987 A, published Aug 5, 1981, and J. J. Baldwin et al., European Patent Application NO. 81102976.8, published Dec. 2, 1981, disclose a number of specific 3,4-disubstituted 1,2,5-thiadiazole-3,4diamine, 1-oxides as inhibitors of gastric acid. The inhibitors function by inhibiting the histamine H-2 receptors. Although N-[2-(dimethylamino)ethyl]-N'-[3-[3-[(1-piperidinyl]methyl]phenoxy ]propyl]- 1,2,5-thiadiazole-3,4-diamine, 1-oxide can be constructed from the generic teachings, it is not exemplified in the numerous examples contained in the above two patents.
We have found N-[2-(dimethylamino)ethyl]-N'-[3-[3-[(1-piperidinyl)- methyl]phenoxy]propyl]-1,2,5-thiadiazole-3,4-diamine, 1-oxide to be an effective inhibitor of histamine H-2 receptors. Investigations with the compound further show that the compound has a specificity of inhibiting gastric acid secretion.
Furthermore, and unexpectedly, the compound has been found to have long acting properties. Consequently, the compound is most suitable as the active ingredient for a "once-a-day" pharmaceutical formulation. These properties, along with a relatively low order of toxicity, render N-[2-(dimethylamino)ethyl] -N'-[3-[3-[(1-piperidinyl)methyl]phenoxyl]propyl]-1,2,5-thiadiazole- 3,4-diamine, 1-oxide as a valuable agent for reducing excesses of gastric acid secretion and for treating ulcers in humans and animals.